Design and development of 2,3-benzodiazepine (CFM) noncompetitive AMPA receptor antagonists

Farmaco. 2002 Feb;57(2):129-34. doi: 10.1016/s0014-827x(01)01186-7.

Abstract

2,3-Benzodiazepines represent a class of heterocyclic compounds that interact with AMPA-type glutamate receptors in a noncompetitive manner. These compounds have attracted great interest for their pharmacological effects against acute and chronic neurodegenerative diseases, such as ischemia and epilepsy. We synthesized a large number of 2,3-benzodiazepine derivatives, which showed anticonvulsant properties in different seizure models and a noncompetitive blockade of AMPA receptor. This article will briefly mention our work in this field and the main SAR considerations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anticonvulsants / chemical synthesis*
  • Anticonvulsants / pharmacology*
  • Anticonvulsants / therapeutic use
  • Benzodiazepines / chemical synthesis*
  • Benzodiazepines / pharmacology*
  • Benzodiazepines / therapeutic use
  • Binding Sites / drug effects
  • Drug Design*
  • Mice
  • Mice, Inbred DBA
  • Molecular Structure
  • Receptors, AMPA / antagonists & inhibitors*
  • Receptors, AMPA / metabolism
  • Seizures / drug therapy
  • Structure-Activity Relationship

Substances

  • Anticonvulsants
  • Receptors, AMPA
  • Benzodiazepines